Imidazoles play an important role in medicinal chemistry, because many of its derivatives have demonstrated significant biological activity. This article is a revision of the last years, of the synthesis methods used in the preparation of imidazole derivatives which have shown biological activity as antibacterial, antiinflammatory, analgesic, antifungal, anticancer, antidepressants, including inside the biological activities of different therapeutic diseases.
Although it is known that the first case of cancer was recorded in ancient Egypt around 1600 BC, it was not until 1917 during the First World War and the development of mustard gas that chemotherapy against cancer became relevant; however, its properties were not recognised until 1946 to later be used in patients. In this sense, the use of metallopharmaceuticals in cancer therapy was extensively explored until the 1960s with the discovery of cisplatin and its anticancer activity. From that date to the present, the search for more effective, more selective metallodrugs with fewer side effects has been an area of continuous exploration. Efforts have led to considering a wide variety of metals from the periodic table, mainly from the d-block, as well as a wide variety of organic ligands, preferably with proven biological activity. In this sense, various research groups have found an ideal binder in Schiff bases, since their raw materials are easily accessible, their synthesis conditions are friendly and their denticity can be manipulated. Therefore, in this review, we have explored the anticancer and antitumor activity reported in the literature for coordination complexes of d-block metals coordinated with tridentate Schiff bases (O N O and O N N) derived from salicylaldehyde. For this work, we have used the main scientific databases CCDC® and SciFinder®.
The synthesis of novel chiral (thio)ureas 1–10 and 14–26 is described. These (thio)ureas incorporate chiral auxiliaries derived from (R)- or (S)-α-phenylethylamine, (R)-phenylglycine, or (1R,2S)-ephedrine. The phenylethyl group in compounds 1–10 and 21–24 adopts a particular orientation in the molecular structure as a consequence of 1,3-allylic strain with the (thio)carbonyl group. Ureas 1–10 were tested as Lewis basic organocatalysts in epoxide ring opening and in aldolic condensation, and it was found that the tetrasubstituted urea (R,R)-2 afforded the best results in terms of reaction yields. (Thio)ureas 20–26 were examined as ligands in the enantioselective diethylzinc addition to benzaldehyde, observing that C2-symmetric chiral urea (R,S,R,S)-20 provides the expected carbinol in nearly quantitative yield and in up to 62% enantiomeric excess.
Throughout human history, bacteria and fungi have caused infections that are difficult to combat. For this reason, countless research groups have developed novel compounds to solve this problem. Thiazole and benzothiazole are present in different structures with interesting biological effects and are used to develop new effective antimicrobial agents. Moreover, nitrogen atoms that are present in this heterocycle allow for coordination with various metals, forming metal complexes that enhance the biological activity of organic ligands that are often used as commercial drugs. This bibliographical review summarizes the copper complexes that use thiazole and benzothiazole as ligands and that report efficient antimicrobial activity against different bacteria and fungi.
Background:
Adjuvants have been obtained empirically by trial and error experiments and
today, there is a tendency to the rational design of adjuvants candidates, which will increasingly
achieve effective and safe products. The aim of this work was to design and evaluate the compound
IMR-23 derived from nitroimidazole as an immunomodulatory molecule.
Material and Methods:
The IMR-23 molecule was obtained by a condensation reaction, cytotoxicity
was tested by the sulforhodamine B assay. Adjuvanticity was evaluated in vivoand in vitroin J774A.1
cells and in the mouse model, respectively.
Results:
IMR-23 that did not show cytotoxicity on HeLa, Vero cells and macrophages J774A.1, was
able to induce the production of molecules involved in the inflammatory process, such as cytokines and
chemokines determined by ELISA, to induce the production of antibodies and to generate antigenspecific
cells to ovalbumin and against the antigen GST-L1b.
Conclusions:
These results open the possibility of further studies to obtain a proper balance of immunogenicity-
toxicity in the use of IMR-23 as an adjuvant molecule.
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